Baricitinib Phosphate
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MedKoo CAT#: 326861

CAS#: 1187595-84-1 (phosphate)

Description: Baricitinib, also known as INCB-028050; INCB-28050; LY-3009104, is an oral highly selective JAK1 and JAK2 inhibitor for inflammatory and autoimmune diseases. There are four known JAK enzymes: JAK1, JAK2, JAK3 and TYK2. JAK-dependent cytokines have been implicated in the pathogenesis of a number of inflammatory and autoimmune diseases, suggesting that JAK inhibitors may be useful for the treatment of a broad range of inflammatory conditions. Baricitinib demonstrates approximately 100-fold greater potency of inhibition against JAK1 and JAK2 than JAK3 in kinase assays.


Price and Availability

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Price

1g
USD 750
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2g
USD 1250
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5g
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Baricitinib Phosphate, purity > 98%, is in stock. purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 326861
Name: Baricitinib Phosphate
CAS#: 1187595-84-1 (phosphate)
Chemical Formula: C16H20N7O6PS
Exact Mass:
Molecular Weight: 469.4128
Elemental Analysis: C, 40.94; H, 4.29; N, 20.89; O, 20.45; P, 6.60; S, 6.83


Related CAS #: 1187594-09-7 (free base)   1187595-84-1 (phosphate)    

Synonym: INCB-028050; INCB-28050; INCB 28050; INCB28050; LY-3009104; LY 3009104; LY3009104; Baricitinib Phosphate.

IUPAC/Chemical Name: (1-(Ethylsulfonyl)-3-(4-(7H-pyrrolo(2,3-d)pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidin-3-yl)ethanenitrile phosphate

InChi Key: FBPOWTFFUBBKBB-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H17N7O2S.H3O4P/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14;1-5(2,3)4/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20);(H3,1,2,3,4)

SMILES Code: N#CCC1(N2N=CC(C3=C4C(NC=C4)=NC=N3)=C2)CN(S(=O)(CC)=O)C1.O=P(O)(O)O


Technical Data

Appearance:
Yellow solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

Related CAS#
CAS#1187594-09-7 (Baricitinib free base)
CAS#1187595-84-1 (Baricitinib Phosphate)


References

1: Nakayamada S, Kubo S, Iwata S, Tanaka Y. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Aug 31. [Epub ahead of print] Review. PubMed PMID: 27577235.

2: Roskoski R Jr. Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases. Pharmacol Res. 2016 Jul 26;111:784-803. doi: 10.1016/j.phrs.2016.07.038. [Epub ahead of print] Review. PubMed PMID: 27473820.

3: Kubo S, Nakayamada S, Tanaka Y. Baricitinib for the treatment of rheumatoid arthritis. Expert Rev Clin Immunol. 2016 Sep;12(9):911-9. doi: 10.1080/1744666X.2016.1214576. Epub 2016 Aug 5. PubMed PMID: 27427830.

4: Tanaka Y. [Tofacitinib for the treatment of rheumatoid arthritis]. Nihon Rinsho. 2016 Jun;74(6):974-80. Review. Japanese. PubMed PMID: 27311188.

5: Perez-Gomez MV, Sanchez-Niño MD, Sanz AB, Zheng B, Martín-Cleary C, Ruiz-Ortega M, Ortiz A, Fernandez-Fernandez B. Targeting inflammation in diabetic kidney disease: early clinical trials. Expert Opin Investig Drugs. 2016 Sep;25(9):1045-58. doi: 10.1080/13543784.2016.1196184. Epub 2016 Jun 13. PubMed PMID: 27268955.

6: Iwata S, Tanaka Y. Progress in understanding the safety and efficacy of Janus kinase inhibitors for treatment of rheumatoid arthritis. Expert Rev Clin Immunol. 2016 Jun 6:1-11. [Epub ahead of print] PubMed PMID: 27253519.

7: Veeraraghavan S, Thappali SR, Viswanadha S, Vakkalanka S, Rangaswamy M. Simultaneous Quantification of Baricitinib and Methotrexate in Rat Plasma by LC-MS/MS: Application to a Pharmacokinetic Study. Sci Pharm. 2016 Apr-Jun;84(2):347-59. doi: 10.3797/scipharm.1510-08. Epub 2015 Dec 20. PubMed PMID: 27222609; PubMed Central PMCID: PMC4871186.

8: Efficacy and Safety of Baricitinib in Japanese Patients with Active Rheumatoid Arthritis Receiving Background Methotrexate Therapy: A 12-week, Double-blind, Randomized Placebo-controlled Study. J Rheumatol. 2016 May;43(5):998. doi: 10.3899/jrheum.150613.C1. PubMed PMID: 27134282.

9: Ummarino D. Rheumatoid arthritis: RA-BEACON illuminates baricitinib. Nat Rev Rheumatol. 2016 Jun;12(6):313. doi: 10.1038/nrrheum.2016.62. Epub 2016 Apr 15. PubMed PMID: 27080693.

10: Genovese MC, Kremer J, Zamani O, Ludivico C, Krogulec M, Xie L, Beattie SD, Koch AE, Cardillo TE, Rooney TP, Macias WL, de Bono S, Schlichting DE, Smolen JS. Baricitinib in Patients with Refractory Rheumatoid Arthritis. N Engl J Med. 2016 Mar 31;374(13):1243-52. doi: 10.1056/NEJMoa1507247. PubMed PMID: 27028914.

11: Yamaoka K. Janus kinase inhibitors for rheumatoid arthritis. Curr Opin Chem Biol. 2016 Jun;32:29-33. doi: 10.1016/j.cbpa.2016.03.006. Epub 2016 Mar 17. Review. PubMed PMID: 26994322.

12: Yiu ZZ, Warren RB. Novel Oral Therapies for Psoriasis and Psoriatic Arthritis. Am J Clin Dermatol. 2016 Jun;17(3):191-200. doi: 10.1007/s40257-016-0179-3. PubMed PMID: 26923915.

13: Tanaka Y, Emoto K, Cai Z, Aoki T, Schlichting D, Rooney T, Macias W. Efficacy and Safety of Baricitinib in Japanese Patients with Active Rheumatoid Arthritis Receiving Background Methotrexate Therapy: A 12-week, Double-blind, Randomized Placebo-controlled Study. J Rheumatol. 2016 Mar;43(3):504-11. doi: 10.3899/jrheum.150613. Epub 2016 Feb 1. PubMed PMID: 26834213.

14: Papp KA, Menter MA, Raman M, Disch D, Schlichting DE, Gaich C, Macias W, Zhang X, Janes JM. A randomized phase 2b trial of baricitinib, an oral Janus kinase (JAK) 1/JAK2 inhibitor, in patients with moderate-to-severe psoriasis. Br J Dermatol. 2016 Jun;174(6):1266-76. doi: 10.1111/bjd.14403. Epub 2016 Apr 5. PubMed PMID: 26800231.

15: Klaeschen AS, Wenzel J. Upcoming therapeutic targets in cutaneous lupus erythematous. Expert Rev Clin Pharmacol. 2016 Feb 29:1-12. [Epub ahead of print] PubMed PMID: 26799969.

16: Jabbari A, Dai Z, Xing L, Cerise JE, Ramot Y, Berkun Y, Sanchez GA, Goldbach-Mansky R, Christiano AM, Clynes R, Zlotogorski A. Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib. EBioMedicine. 2015 Feb 26;2(4):351-5. doi: 10.1016/j.ebiom.2015.02.015. eCollection 2015 Apr. PubMed PMID: 26137574; PubMed Central PMCID: PMC4486197.

17: Khan IM, Perrard XY, Brunner G, Lui H, Sparks LM, Smith SR, Wang X, Shi ZZ, Lewis DE, Wu H, Ballantyne CM. Intermuscular and perimuscular fat expansion in obesity correlates with skeletal muscle T cell and macrophage infiltration and insulin resistance. Int J Obes (Lond). 2015 Nov;39(11):1607-18. doi: 10.1038/ijo.2015.104. Epub 2015 Jun 4. PubMed PMID: 26041698; PubMed Central PMCID: PMC5007876.

18: Keystone EC, Taylor PC, Drescher E, Schlichting DE, Beattie SD, Berclaz PY, Lee CH, Fidelus-Gort RK, Luchi ME, Rooney TP, Macias WL, Genovese MC. Safety and efficacy of baricitinib at 24 weeks in patients with rheumatoid arthritis who have had an inadequate response to methotrexate. Ann Rheum Dis. 2015 Feb;74(2):333-40. doi: 10.1136/annrheumdis-2014-206478. Epub 2014 Nov 27. PubMed PMID: 25431052; PubMed Central PMCID: PMC4316868.

19: Shi JG, Chen X, Lee F, Emm T, Scherle PA, Lo Y, Punwani N, Williams WV, Yeleswaram S. The pharmacokinetics, pharmacodynamics, and safety of baricitinib, an oral JAK 1/2 inhibitor, in healthy volunteers. J Clin Pharmacol. 2014 Dec;54(12):1354-61. doi: 10.1002/jcph.354. PubMed PMID: 24965573.

20: Norman P. Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77. doi: 10.1517/13543784.2014.918604. Epub 2014 May 12. Review. PubMed PMID: 24818516.